The development of novel inhibitors of tumor necrosis factor-α (TNF-α) production based on substituted [5,5]-bicyclic pyrazolones
2004
Abstract Novel substituted [5,5]-bicyclic pyrzazolones are presented as inhibitors of tumor necrosis factor-α (TNF-α) production. Many of these compounds show low nanomolar activity against lipopolysaccaride (LPS)-induced TNF-α production in THP-1 cells. This class of molecules was co-crystallized with mutated p38, and several analogs showed good oral bioavailability in the rat. Oral activity of these compounds in the rat iodoacetate model for osteoarthritis is discussed.
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